PXR, CAR and drug metabolism

被引：400
作者：
Willson, TM [1 ]
Kliewer, SA [1 ]
机构：
[1] GlaxoSmithKline, Discovery Res, Res Triangle Pk, NC 27709 USA
来源：
NATURE REVIEWS DRUG DISCOVERY | 2002年 / 1卷 / 04期
关键词：
D O I：
10.1038/nrd753
中图分类号：
Q81 [生物工程学（生物技术）]; Q93 [微生物学];
学科分类号：
071005 ; 0836 ; 090102 ; 100705 ;
摘要：
Mechanisms that protect the body from a diverse array of harmful chemicals are also involved in drug metabolism, and can cause adverse drug-drug interactions. Two closely related orphan nuclear hormone receptors - the pregnane X receptor (PXR) and the constitutive androstane receptor (CAR) - have recently emerged as transcriptional regulators of cytochrome P450 expression that couple xenobiotic exposure to oxidative metabolism. In this review, we provide an examination of the roles of PXR and CAR as xenobiotic sensors, and discuss the application of this knowledge to toxicological screening in drug discovery.
引用
收藏
页码：259 / 266
页数：8
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